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Volume 14
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10.3390/ECMC2022-13172
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Abstract

Synthesis of Novel 2-Phenylindole Analogues as Antifungal and Antibacterial Agents †

by
Ke Yang
and
Xinhui Pan
*
Laboratory of Xinjiang Phytomedicine Resource and Utilization, Ministry of Education, School of Pharmaceutical Sciences, Shihezi University, Shihezi 832002, China
*
Author to whom correspondence should be addressed.
†
Presented at the 8th International Electronic Conference on Medicinal Chemistry, 1–30 November 2022; Available online: https://ecmc2022.sciforum.net/.
Med. Sci. Forum 2022, 14(1), 128; https://doi.org/10.3390/ECMC2022-13172
Published: 1 November 2022
(This article belongs to the Proceedings of The 8th International Electronic Conference on Medicinal Chemistry)
Versions Notes

Abstract

:
A series of novel indole derivatives containing ester groups, halogen, epoxy and short-chain aliphatic hydrocarbons were designed, synthesized and evaluated for their antibacterial activities. Most of the compounds showed relatively excellent inhibitory activities against different strains (including a multidrug-resistant clinical isolate). Compounds 3f, 3o and 3r showed the strongest inhibitory activity (mic of 2–32 μg/mL). Compounds 3f, 3h, 3i, 3o and 3r with antibacterial activity were not cytotoxic against RAW 264.7 mouse macrophages. The structure–activity relationship analysis and docking studies showed that the halogens as well as aliphatic hydrocarbons could enhance the antibacterial ability and reduce the toxicity of the indole compounds.

Supplementary Materials

The following are available online at https://www.mdpi.com/article/10.3390/ECMC2022-13172/s1.

Author Contributions

Conceptualization, X.P.; methodology, X.P.; experiment, K.Y., software, K.Y.; validation, X.P.; formal analysis, K.Y.; investigation, K.Y.; resources, K.Y.; data curation, K.Y.; writing—original draft preparation, K.Y.; writing—review and editing, X.P.; supervision, X.P. All authors have read and agreed to the published version of the manuscript.

Funding

This study was supported by National Natural Science Foundation of China (82160651); The Open Project of Stake Key Laboratory of Natural and Biomimetic Drugs, Peking University (K202103); The Open Project of Key Laboratory of Xinjiang Phytomedicine Resource and Utilization, Ministry of Education (XPRU202004); Youth Innovative Talent Cultivation Projects of Shihezi University (CXPY202005) and The Open Sharing Fund for the Large-scale Instruments and Equipments of Shihezi University.

Institutional Review Board Statement

The animal study protocol was approved by the Ethics Committee of the First Affiliated Hospital, School of Medicine, Shihezi University (protocol code A2022-209-01).

Informed Consent Statement

Not applicable.

Data Availability Statement

The data presented in this study are available in the article.

Conflicts of Interest

The authors declare no conflict of interest.
Publisher’s Note: MDPI stays neutral with regard to jurisdictional claims in published maps and institutional affiliations.
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Share and Cite

MDPI and ACS Style

Yang, K.; Pan, X. Synthesis of Novel 2-Phenylindole Analogues as Antifungal and Antibacterial Agents. Med. Sci. Forum 2022, 14, 128. https://doi.org/10.3390/ECMC2022-13172

AMA Style

Yang K, Pan X. Synthesis of Novel 2-Phenylindole Analogues as Antifungal and Antibacterial Agents. Medical Sciences Forum. 2022; 14(1):128. https://doi.org/10.3390/ECMC2022-13172

Chicago/Turabian Style

Yang, Ke, and Xinhui Pan. 2022. "Synthesis of Novel 2-Phenylindole Analogues as Antifungal and Antibacterial Agents" Medical Sciences Forum 14, no. 1: 128. https://doi.org/10.3390/ECMC2022-13172

APA Style

Yang, K., & Pan, X. (2022). Synthesis of Novel 2-Phenylindole Analogues as Antifungal and Antibacterial Agents. Medical Sciences Forum, 14(1), 128. https://doi.org/10.3390/ECMC2022-13172

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